Schistosomiasis is a notable neglected tropical disease caused by trematodes that infect
mainly the intestines, bladder, and liver. Because of the unavailability of a schistosomiasis vaccine,
control of the disease depends mainly on chemotherapy. Praziquantel (PZQ), which is active against all
schistosome species (Among the five major species of human schistosomes−S. mansoni, S.
haematobium, S. japonicum, S. intercalatum, and S. mekongi, S. mansoni is the most prevalent) as well
as probably their hybrids and the recommended drug by the World Health Organization for
schistosomiasis treatment at either the community or individual level, has become the exclusive drug
because of its low cost and efficacy against the adult form of all schistosome species. In view of rapid
re-infection following treatment and concern about the development of tolerance and/or resistance to
praziquantel, there is an urgent need for research and development of novel drugs for the prevention and
treatment of schistosomiasis. This comprehensive review shall attempt to briefly review the recent
advances in the synthesis of antischistosomal drugs and agents in the literature from 1990s to now,
particularly focusing on the context of potential development of antischistosomal agents. It shall be of
interest for the pharmacologist.